Assay Detail
Binding
CHEMBL5733274
Review assay metadata, readout intent, target linkage, and publication context from the same page.
p38 MAPKgamma Enzyme Inhibition: The inhibitory activities of compounds of the invention against p38MAPKγ (MAPK12: Invitrogen), were evaluated in a similar fashion to that described hereinabove. The enzyme (800 ng/mL, 2.5 μL) was incubated with the test compound (2.5 μL at either 4 μg/mL, 0.4 μg/mL, 0.04 μg/mL, or 0.004 μg/mL) for 2 hr at RT. The FRET peptides (8 μM, 2.5 μL), and appropriate ATP solution (2.5 μL, 400 μM) was then added to the enzymes/compound mixtures and incubated for 1 hr. Development reagent (protease, 5 μL) was added for 1 hr prior to detection in a fluorescence microplate reader (Varioskan® Flash, Thermo Scientific).
108
Total Activities
32
Compounds Tested
4
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1-pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl) oxy) napththalen-1-yl) ureas as p38 MAP kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| kon | 36 | - | - |
| k_off | 36 | - | - |
| IC50 | 34 | 6.07 | 6.58 |
| Kd | 2 | 7.84 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3695569 | — | — | 6 | 8.30 |
| CHEMBL3701217 | — | — | 6 | 7.37 |
| CHEMBL5768918 | — | — | 3 | 6.58 |
| CHEMBL5951223 | — | — | 3 | 6.55 |
| CHEMBL5988695 | — | — | 3 | 6.37 |
| CHEMBL5848716 | — | — | 3 | 6.27 |
| CHEMBL5896412 | — | — | 6 | 6.25 |
| CHEMBL5794070 | — | — | 3 | 6.16 |
| CHEMBL6043284 | — | — | 3 | 5.82 |
| CHEMBL5896806 | — | — | 3 | 5.77 |
| CHEMBL6014943 | — | — | 3 | 5.09 |
| CHEMBL5820343 | — | — | 3 | - |
| CHEMBL5853055 | — | — | 3 | - |
| CHEMBL6007304 | — | — | 3 | - |
| CHEMBL5921712 | — | — | 3 | - |
| CHEMBL5756167 | — | — | 3 | - |
| CHEMBL5947021 | — | — | 3 | - |
| CHEMBL6019442 | — | — | 3 | - |
| CHEMBL5762929 | — | — | 3 | - |
| CHEMBL5977979 | — | — | 3 | - |
| CHEMBL6008491 | — | — | 3 | - |
| CHEMBL5830994 | — | — | 3 | - |
| CHEMBL5761911 | — | — | 3 | - |
| CHEMBL5754667 | — | — | 3 | - |
| CHEMBL5896751 | — | — | 6 | - |
| CHEMBL5901318 | — | — | 3 | - |
| CHEMBL5836383 | — | — | 3 | - |
| CHEMBL5758982 | — | — | 3 | - |
| CHEMBL6035491 | — | — | 3 | - |
| CHEMBL6014353 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3695569 | — | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL3701217 | — | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL5768918 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL5951223 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL3695569 | — | IC50 | = | 344.0 | nM | 6.46 |
| CHEMBL5988695 | — | IC50 | = | 423.0 | nM | 6.37 |
| CHEMBL5848716 | — | IC50 | = | 535.0 | nM | 6.27 |
| CHEMBL5896412 | — | IC50 | = | 557.0 | nM | 6.25 |
| CHEMBL5794070 | — | IC50 | = | 695.0 | nM | 6.16 |
| CHEMBL5896412 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL6043284 | — | IC50 | = | 1503.0 | nM | 5.82 |
| CHEMBL5896806 | — | IC50 | = | 1702.0 | nM | 5.77 |
| CHEMBL3701217 | — | IC50 | = | 3739.0 | nM | 5.43 |
| CHEMBL6014943 | — | IC50 | = | 8198.0 | nM | 5.09 |
| CHEMBL5951223 | — | k_off | = | - | s-1 | - |
| CHEMBL5921712 | — | IC50 | > | 15800.0 | nM | - |
| CHEMBL5830994 | — | IC50 | > | 1630.0 | nM | - |
| CHEMBL5830994 | — | kon | = | - | — | - |
| CHEMBL5836383 | — | IC50 | > | 1580.0 | nM | - |
| CHEMBL3695569 | — | k_off | = | - | s-1 | - |
| CHEMBL3695569 | — | kon | = | - | — | - |
| CHEMBL3701217 | — | k_off | = | - | s-1 | - |
| CHEMBL3701217 | — | kon | = | - | — | - |
| CHEMBL5768918 | — | k_off | = | - | s-1 | - |
| CHEMBL5768918 | — | kon | = | - | — | - |
| CHEMBL5758982 | — | k_off | = | - | s-1 | - |
| CHEMBL5758982 | — | kon | = | - | — | - |
| CHEMBL5758982 | — | IC50 | > | 1620.0 | nM | - |
| CHEMBL5836383 | — | k_off | = | - | s-1 | - |
| CHEMBL5836383 | — | kon | = | - | — | - |
| CHEMBL5754667 | — | IC50 | > | 1540.0 | nM | - |
| CHEMBL5754667 | — | k_off | = | - | s-1 | - |
| CHEMBL5947021 | — | k_off | = | - | s-1 | - |
| CHEMBL5754667 | — | kon | = | - | — | - |
| CHEMBL5896751 | — | kon | = | - | — | - |
| CHEMBL5896751 | — | k_off | = | - | s-1 | - |
| CHEMBL5756167 | — | IC50 | > | 16000.0 | nM | - |
| CHEMBL5756167 | — | kon | = | - | — | - |
| CHEMBL5756167 | — | k_off | = | - | s-1 | - |
| CHEMBL5947021 | — | IC50 | > | 1670.0 | nM | - |
| CHEMBL5947021 | — | kon | = | - | — | - |
| CHEMBL5951223 | — | kon | = | - | — | - |
| CHEMBL6019442 | — | IC50 | > | 1590.0 | nM | - |
| CHEMBL6019442 | — | kon | = | - | — | - |
| CHEMBL6019442 | — | k_off | = | - | s-1 | - |
| CHEMBL6014353 | — | IC50 | > | 1660.0 | nM | - |
| CHEMBL6014353 | — | kon | = | - | — | - |
| CHEMBL6014353 | — | k_off | = | - | s-1 | - |
| CHEMBL5794070 | — | kon | = | - | — | - |
| CHEMBL5794070 | — | k_off | = | - | s-1 | - |